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某些立体异构稠合1,3-恶嗪-4-酮的合成、构象及药理作用。44:立体化学研究;22:饱和杂环

[Synthesis, conformation and pharmacological effect of some stereoisomeric condensed 1,3-oxazine-4-ones. 44: Stereochemical studies; 22: Saturated heterocycles].

作者信息

Bernáth G, Fülöp F, Ecsery Z, Blazsó G, Minker E

出版信息

Pharmazie. 1983 Feb;38(2):89-92.

PMID:6602344
Abstract

It has been reported the synthesis, examination of the stereochemistry and biological effect of 2-substituted-cis-5,6-trimethylen-, cis- and trans-5,6-tetramethylene and -5,6-pentamethylene-2,3,5,6-tetrahydro-1,3-oxazine-4-one derivatives. Primarily cis-isomers were synthetized because in the pharmacological test systems the trans isomers were less active. The compounds tested have an antiphlogistic effect of different intrinsic activity.

摘要

据报道,已合成了2-取代-顺式-5,6-亚甲基、顺式和反式-5,6-四亚甲基以及-5,6-五亚甲基-2,3,5,6-四氢-1,3-恶嗪-4-酮衍生物,并对其立体化学和生物学效应进行了研究。主要合成的是顺式异构体,因为在药理测试系统中反式异构体活性较低。所测试的化合物具有不同内在活性的抗炎作用。

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